Water-soluble compositions of bioactive lipophilic compounds
AssigneeNational Research Council of Canada
InventorsHenryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
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AssigneeNational Research Council of Canada
InventorsHenryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
Estimating the term…
Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula: {X—OOC—[(CH2)n—COO]m}p—Y (I) wherein: X is a residue of a hydrophobic moiety, Y is a residue of a hydrophilic moiety, p is 1 or 2, m is 0 or 1, and n is an integer greater than or equal to 0 are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In some embodiments, the sterol is cholesterol or sitosterol, the tocopherol is α-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 400 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.
A method for the treatment of a fungal infection in humans or warm-blooded animals in need of such treatment, comprising administering to such human or warm-blooded animal, a therapeutically effective amount of a water-soluble composition, comprising a solubilizing agent selected from the group consisting of polyoxyethanyl-sitosterol sebacate, polyoxyethanyl-cholesteryl sebacate and polyoxyethanyl-α-tocopheryl sebacate, and a macrolide polyene antibiotic, formulated in a weight ratio of solubilizing agent to antibiotic of 2:1 to 4:1, in conjunction with a pharmaceutically effective carrier or excipient.
A water-soluble composition, comprising a solubilizing agent selected from the group consisting of polyoxyethanyl-sitosterol sebacate, polyoxyethanyl-cholesteryl sebacate and polyoxyethanyl-α-tocopheryl sebacate, and a macrolide polyene antibiotic, formulated in a weight ratio of solubilizing agent to antibiotic of 2:1 to 4:1.
Dependencies are inferred from the claim text.